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PE20142182A1 - IAP INHIBITORS - Google Patents

IAP INHIBITORS

Info

Publication number
PE20142182A1
PE20142182A1 PE2014001069A PE2014001069A PE20142182A1 PE 20142182 A1 PE20142182 A1 PE 20142182A1 PE 2014001069 A PE2014001069 A PE 2014001069A PE 2014001069 A PE2014001069 A PE 2014001069A PE 20142182 A1 PE20142182 A1 PE 20142182A1
Authority
PE
Peru
Prior art keywords
iap inhibitors
refers
compound
iap
inhibitors
Prior art date
Application number
PE2014001069A
Other languages
Spanish (es)
Inventor
Frederick Cohen
Lewis J Gazzard
Vickie Hsiao-Wei Tsui
John A Flygare
Original Assignee
Curis Inc
Genentech Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Curis Inc, Genentech Inc filed Critical Curis Inc
Publication of PE20142182A1 publication Critical patent/PE20142182A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06Tripeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/4211,3-Oxazoles, e.g. pemoline, trimethadione
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0812Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0815Tripeptides with the first amino acid being basic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

SE REFIERE AL COMPUESTO (2-OXAZOL-2-IL-4-FENIL-TIAZOL-5-IL)-AMIDA DEL ACIDO (S)-1-[(S)-2-CICLOHEXIL-2-((S)-2-METILAMINO-PROPIONILAMINO)-ACETIL]-PIRROLIDIN-2-CARBOXILICO. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES UN INHIBIDOR DE IAP (INHIBIDORES DE APOPTOSIS) QUE ES UTIL EN EL TRATAMIENTO DEL CANCER.REFERS TO THE COMPOUND (2-OXAZOL-2-IL-4-PHENYL-THIAZOL-5-IL) -AMIDE OF ACID (S) -1 - [(S) -2-CYCLOHEXIL-2 - ((S) -2 -METILAMINO-PROPIONYLAMINO) -ACETIL] -PIRROLIDIN-2-CARBOXILICO. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. SAID COMPOUND IS AN INHIBITOR OF IAP (INHIBITORS OF APOPTOSIS) THAT IS USEFUL IN THE TREATMENT OF CANCER.

PE2014001069A 2012-01-03 2013-01-03 IAP INHIBITORS PE20142182A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261582760P 2012-01-03 2012-01-03

Publications (1)

Publication Number Publication Date
PE20142182A1 true PE20142182A1 (en) 2015-01-16

Family

ID=48695302

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2014001069A PE20142182A1 (en) 2012-01-03 2013-01-03 IAP INHIBITORS

Country Status (41)

Country Link
US (6) US8716236B2 (en)
EP (2) EP2800749B1 (en)
JP (2) JP5747137B2 (en)
KR (3) KR101855566B1 (en)
CN (2) CN107915728B (en)
AR (2) AR089623A1 (en)
AU (1) AU2013202780B2 (en)
BR (1) BR112014016637B1 (en)
CA (1) CA2861637C (en)
CL (1) CL2014001770A1 (en)
CO (1) CO7020915A2 (en)
CR (1) CR20140367A (en)
CY (2) CY1118371T1 (en)
DK (2) DK2800749T3 (en)
EC (1) ECSP14011792A (en)
ES (2) ES2594856T3 (en)
HK (1) HK1203949A1 (en)
HR (2) HRP20161381T1 (en)
HU (2) HUE037760T2 (en)
IL (2) IL242314A (en)
LT (2) LT2800749T (en)
MA (1) MA35895B1 (en)
ME (2) ME03084B (en)
MX (1) MX336294B (en)
MY (1) MY178390A (en)
NO (1) NO2755614T3 (en)
NZ (1) NZ627480A (en)
PE (1) PE20142182A1 (en)
PH (2) PH12014501534B1 (en)
PL (2) PL2800749T3 (en)
PT (2) PT2800749T (en)
RS (2) RS57438B1 (en)
RU (2) RU2593259C2 (en)
SG (1) SG11201403784QA (en)
SI (2) SI3133073T1 (en)
SM (2) SMT201800352T1 (en)
TR (1) TR201808088T4 (en)
TW (1) TWI503318B (en)
UA (1) UA114417C2 (en)
WO (1) WO2013103703A1 (en)
ZA (1) ZA201405535B (en)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NO2755614T3 (en) 2012-01-03 2018-03-31
WO2016079527A1 (en) 2014-11-19 2016-05-26 Tetralogic Birinapant Uk Ltd Combination therapy
WO2016097773A1 (en) 2014-12-19 2016-06-23 Children's Cancer Institute Therapeutic iap antagonists for treating proliferative disorders
CN109705191B (en) * 2017-10-25 2022-04-29 广东东阳光药业有限公司 IAP inhibitor and its application in medicine
CN114685602A (en) * 2017-11-13 2022-07-01 正大天晴药业集团股份有限公司 SMAC mimetics useful as IAP inhibitors and uses thereof
WO2020027225A1 (en) 2018-07-31 2020-02-06 ファイメクス株式会社 Heterocyclic compound
JP7764027B2 (en) 2019-07-31 2025-11-05 ファイメクス株式会社 heterocyclic compounds
CN112972684B (en) * 2019-12-02 2024-05-31 苏州亚盛药业有限公司 Combination of IAP inhibitors with PARP or MEK inhibitors or other chemotherapeutic agents
KR20220130190A (en) 2020-01-20 2022-09-26 아스트라제네카 아베 Epidermal growth factor receptor tyrosine kinase inhibitor for cancer treatment
KR20240132251A (en) 2021-10-22 2024-09-03 유니버시티 오브 휴스턴 시스템 Methods and compositions for treating chronic inflammatory damage, metaplasia, dysplasia and cancer of epithelial tissue
CN117110469B (en) * 2023-08-18 2025-12-09 中国检验检疫科学研究院 Method for determining forbidden components in anti-hair loss cosmetics

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US4526988A (en) 1983-03-10 1985-07-02 Eli Lilly And Company Difluoro antivirals and intermediate therefor
WO1998046576A2 (en) 1997-04-15 1998-10-22 Genentech, Inc. Halo-alkoxycarbonyl prodrugs
NZ588799A (en) * 2004-07-02 2012-06-29 Genentech Inc Inhibitors of iap
DE602005022936D1 (en) * 2004-12-20 2010-09-23 Genentech Inc PYRROLIDINES AS INHIBITORS OF IAP
CN101595121A (en) 2006-10-12 2009-12-02 诺瓦提斯公司 Pyrrolidin derivatives as the IAP inhibitor
AR066348A1 (en) 2007-04-30 2009-08-12 Genentech Inc IAP INHIBITORS
NO2755614T3 (en) * 2012-01-03 2018-03-31
USD690416S1 (en) 2012-12-12 2013-09-24 Pharmajet, Inc. Needle-free syringe

Also Published As

Publication number Publication date
PT2800749T (en) 2016-10-24
RU2728789C2 (en) 2020-07-31
EP3133073A3 (en) 2017-03-22
CO7020915A2 (en) 2014-08-11
RS57438B1 (en) 2018-09-28
PH12015501038A1 (en) 2015-09-21
SG11201403784QA (en) 2014-08-28
CN107915728A (en) 2018-04-17
US20220211797A1 (en) 2022-07-07
US20130172264A1 (en) 2013-07-04
MX336294B (en) 2016-01-14
US11096982B2 (en) 2021-08-24
WO2013103703A1 (en) 2013-07-11
KR101855566B1 (en) 2018-05-04
KR101553792B1 (en) 2015-09-16
EP2800749A1 (en) 2014-11-12
HRP20180976T1 (en) 2018-08-10
PH12014501534A1 (en) 2014-10-08
IL242314A (en) 2016-08-31
SI3133073T1 (en) 2018-06-29
KR20180051646A (en) 2018-05-16
US20160102119A1 (en) 2016-04-14
HUE031305T2 (en) 2017-07-28
TW201333001A (en) 2013-08-16
PH12015501038B1 (en) 2015-09-21
CA2861637C (en) 2017-07-18
TR201808088T4 (en) 2018-06-21
BR112014016637A2 (en) 2017-06-13
ES2672809T3 (en) 2018-06-18
LT3133073T (en) 2018-06-25
SI2800749T1 (en) 2016-11-30
PL2800749T3 (en) 2017-01-31
IL233386A0 (en) 2014-08-31
NZ627480A (en) 2016-04-29
SMT201600357B (en) 2016-11-10
US8716236B2 (en) 2014-05-06
AU2013202780B2 (en) 2015-04-16
KR101917992B1 (en) 2018-11-13
RU2016124658A3 (en) 2019-09-09
PH12014501534B1 (en) 2014-10-08
CL2014001770A1 (en) 2015-04-17
US9586991B2 (en) 2017-03-07
TWI503318B (en) 2015-10-11
PL3133073T3 (en) 2018-09-28
JP2015199738A (en) 2015-11-12
MA35895B1 (en) 2014-12-01
EP2800749A4 (en) 2015-08-05
HK1203949A1 (en) 2015-11-06
RU2014130171A (en) 2016-02-27
RU2593259C2 (en) 2016-08-10
ZA201405535B (en) 2017-08-30
ES2594856T3 (en) 2016-12-23
PT3133073T (en) 2018-06-18
CN104159897A (en) 2014-11-19
US20140235551A1 (en) 2014-08-21
US9238675B2 (en) 2016-01-19
ECSP14011792A (en) 2015-12-31
KR20140107670A (en) 2014-09-04
MY178390A (en) 2020-10-12
ME02526B (en) 2017-02-20
UA114417C2 (en) 2017-06-12
EP3133073A2 (en) 2017-02-22
HRP20161381T1 (en) 2016-12-02
SMT201800352T1 (en) 2018-09-13
BR112014016637A8 (en) 2017-07-04
MX2014007895A (en) 2015-03-19
KR20150065960A (en) 2015-06-15
EP2800749B1 (en) 2016-09-21
AR123542A2 (en) 2022-12-14
NO2755614T3 (en) 2018-03-31
DK2800749T3 (en) 2016-11-07
US11963994B2 (en) 2024-04-23
JP5747137B2 (en) 2015-07-08
US20190224269A1 (en) 2019-07-25
LT2800749T (en) 2016-10-25
RS55327B1 (en) 2017-03-31
US20170136084A1 (en) 2017-05-18
IL233386A (en) 2016-08-31
CN107915728B (en) 2021-04-30
ME03084B (en) 2019-01-20
BR112014016637B1 (en) 2022-06-14
HUE037760T2 (en) 2018-09-28
DK3133073T3 (en) 2018-06-18
AU2013202780A1 (en) 2013-07-18
RU2016124658A (en) 2018-12-04
AR089623A1 (en) 2014-09-03
CA2861637A1 (en) 2013-07-11
EP3133073B1 (en) 2018-05-02
JP2015504072A (en) 2015-02-05
CR20140367A (en) 2015-02-18
CY1118371T1 (en) 2017-06-28
CY1120355T1 (en) 2019-07-10

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